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Gumetinib is a potent, highly selective, and brain-penetrant small molecule inhibitor of the mesenchymal-epithelial transition (MET) receptor tyrosine kinase. Developed by the Shanghai Institute of Materia Medica (SIMM) in collaboration with Haihe Biopharma, it is specifically designed to target MET alterations, such as MET exon 14 skipping mutations, which are key oncogenic drivers in a subset of non-small cell lung cancers (NSCLC). Gumetinib demonstrates significant antitumor activity by blocking MET-mediated signaling pathways, including those involved in cell proliferation, survival, and metastasis. It received conditional approval from China's National Medical Products Administration (NMPA) in March 2023 for the treatment of adult patients with locally advanced or metastatic NSCLC harboring MET exon 14 skipping mutations. Its ability to cross the blood-brain barrier makes it a promising therapeutic option for patients with central nervous system metastases.
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